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Abstract：
Both c-Met and VEGFR-2 were important targets for cancer therapies. In order to develop reversible and non-covalent c-Met and VEGFR-2 dual inhibitors, a series of [1,4] dioxino[2,3-f] quinazoline derivatives were designed and synthesized. The enzyme assay demonstrated that most target compounds had inhibition potency on both c-Met and VEGFR-2 with IC50 values in nanomolar range especially compounds 7m and 7k. Based on further cell proliferation assay in vitro, compound 7k showed significantly anti-tumor activity in vivo on a hepatocellular carcinoma (MHCC97H cells) xenograft mouse model. We docked the compound 7m with c-Met and VEGFR-2 kinases, and interpreted the SAR of these analogues. All results indicated that the target compounds were dual inhibitors of c-Met and VEGFR-2 kinases that held promising potential in cancer therapy.
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BIOORGANIC CHEMISTRY
ISSN： 0045-2068
Year： 2019
Volume： 88
5 . 1 0 0
JCR@2022
ESI Discipline： BIOLOGY & BIOCHEMISTRY;
ESI HC Threshold：169
JCR Journal Grade：1
Cited Count：
WoS CC Cited Count： 29
SCOPUS Cited Count： 28
ESI Highly Cited Papers on the List： 0 Unfold All
WanFang Cited Count：
Chinese Cited Count：
30 Days PV： 7
